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1

Gordon, Nathaniel Charles. "Protease engineering for therapeutic applications." Thesis, University of Cambridge, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.648185.

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2

Vigne, Aurélie. "Microfluidic tools for the engineering of enzymes of therapeutic interest." Thesis, Bordeaux, 2018. http://www.theses.fr/2018BORD0391/document.

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Cette thèse concerne le développement d’outils microfluidique pour l’ingénierie d’enzymes d’intérêt thérapeutique. La microfluidique à base de gouttelettes présente un énorme potentiel dans le domaine de la biologie quantitative. Nous développons des outils microfluidiques pour l’évolution dirigée de l’enzyme L-asparaginase, enzyme utilisée comme traitement de laleucémie lymphoblastique aiguë. Ce traitement est basée sur une enzyme d’origine bactérienne,ce qui conduit à déclencher des réactions immunitaires qui se traduit par l’interruption du traitement, souvent fatale pour le patient. Cepend
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3

Lovering, Andrew Lee. "X-ray crystallographic studies of therapeutic enzymes : nitroreductase and AKR1C3." Thesis, University of Birmingham, 2003. http://etheses.bham.ac.uk//id/eprint/3588/.

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The \(Escherichia\) \(coli\) enzyme nitroreductase has been proposed as a candidate for the Gene-Directed Enzyme Prodrug Therapy approach in treating cancer. Structural studies on the enzyme were instigated in a first step towards improving enzyme activity. The enzyme was crystallized with the substrate analogue, nicotinic acid, and the structures of three crystal forms obtained. The fold has a mixed a/P structure, with a molecule of nicotinic acid bound next to the FMN cofactor. Several active site residues were identified as candidates for mutation. This procedure produced many mutant enzyme
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4

Guiney, Daniel. "Design and synthesis of inhibitors of enzymes in the folate biosynthesis pathway." Thesis, University of Strathclyde, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.273387.

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5

Hart, R. J. "Developing protein conjugation techniques to enhance cell delivery of therapeutic enzymes." Thesis, University of Sheffield, 2017. http://etheses.whiterose.ac.uk/18996/.

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The focus of disease research often surrounds therapeutic pathway identification and the subsequent investigation of proteins or compounds that potentially interfere with disease mechanisms. However, finding targets and effective therapeutic domains often overshadows another important aspect of drug delivery and efficacy; the method of domain conjugation. Unfortunately the combination of good therapeutic components and good therapeutic design can often be amiss, with differing skills and groups needed to marry the two together. In recognition of this, there are new techniques emerging that aim
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6

Maheshwari, Sweta. "Caractérisation biochimique et cellulaire des enzymes clés du métabolisme des phospholipides chez Plasmodium falciparum." Thesis, Montpellier 2, 2012. http://www.theses.fr/2012MON20004.

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Le développement du parasite Plasmodium falciparum, responsable du paludisme, nécessite la synthèse de phospholipides et plus particulièrement de phosphatidylcholine (PC) et phosphaditylethanolamine (PE) qui représentent environ 85% de la totalité des phospholidipes du parasite. Leur synthèse s'effectue principalement par les voies métaboliques de novo, voies de Kennedy, en trois étapes enzymatiques. Les enzymes CTP: phosphoethanolamine cytidylyltransferase (ECT) et CTP: phosphocholine cytidylyltransferase (CCT) catalysent les étapes limitantes des deux voies de biosynthèse de la PE et de la P
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7

Mao, Wei. "Etude biochimique et sélection d'inhibiteurs spécifiques d'une cible thérapeutique leishmanienne : la GDP-Mannose-Pyrophosphorylase." Thesis, Université Paris-Saclay (ComUE), 2016. http://www.theses.fr/2016SACLS481.

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Les leishmanioses sont des maladies tropicales négligées provoquées par un protozoaire parasite du genre Leishmania, et transmises par un insecte vecteur, le phlébotome. Les leishmanioses menacent 310 millions de personnes dans 98 pays à travers le monde. Les traitements antileishmaniens actuels sont limités et présentent des problèmes majeurs de toxicité et d'émergence de chimiorésistance. Dans ce contexte, il est nécessaire de développer de nouveaux agents antileishmaniens spécifiquement dirigés contre une cible thérapeutique chez le parasite. La GDP-Mannose Pyrophosphorylase (GDP-MP) est un
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8

AIELLO, ROSANNA GILDA. "IMPROVING THE THERAPEUTIC POTENTIAL OF LYSOSOMAL ENZYMES TO TREAT CNS IN LYSOSOMAL STORAGE DISORDERS." Doctoral thesis, Università degli Studi di Milano, 2020. http://hdl.handle.net/2434/793420.

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Lysosomal storage disorders (LSD) are a large group of inherited genetic diseases caused by impaired activity of lysosomal enzymes leading to accumulation of undigested macromolecules within the lysosomes and thus cell dysfunction. The clinical manifestation is heterogeneous and neurological involvement represents a major problem. The correction of the defective gene/protein represents the primary strategy for the treatment of these genetic conditions. However, the clinical translation of these approaches is very challenging because of the difficulty in achieving and maintaining therapeutic
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9

Mendieta, Martínez Laura. "Protease inhibitors as therapeutic agents." Doctoral thesis, Universitat de Barcelona, 2014. http://hdl.handle.net/10803/279388.

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Proteases are involved in a high number of diseases, and thus, are relevant targets. For that reason our main goal was the discovery of protease inhibitors as therapeutic agents. We focused our study in four proteases: dipeptidyl peptidase IV (diabetes mellitus type 2), prolyl oligopeptidase (cognitive disorders) and cathepsins L and B (cancer).For the discovery of inhibitors, three strategies were selected: medicinal plant screening, high throughput screening and the characterization of a combinatorial chemistry library. Once accomplished the DPP IV recombinant expression optimization, t
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10

Mirza, Ahmad. "Structural characterization of novel antimicrobial therapeutic targets and crystallographic examination of enzymes involved in xenobiotic metabolism." Thesis, McGill University, 2010. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=86555.

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Part I. Recently there has been an alarming rise in the number of infections due to pathogenic organisms that are insensitive to our current arsenal of pharmaceuticals, necessitating the identification of new antimicrobial targets. Here, we describe structural studies of two enzymes from the aspartate family of biosynthetic enzymes in order to assess their potential for drug targeting. Our first report details how an unlikely inhibitor with low millimolar binding characteristics, 5-hydroxy-4-oxo-norvaline, can effectively inactivate homoserine dehydrogenase (HSD) through the formation of a tig
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11

Chen, Shen-En Trawick Mary Lynn. "Modeling, design, and development of potential inhibitors of [gamma]-glutamylamine cyclotransferase and inhibitors of cruzain as therapeutic agents for Chagas' disease." Waco, Tex. : Baylor University, 2008. http://hdl.handle.net/2104/5189.

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12

Saliba, Mineem. "Recherche de nouvelles stratégies thérapeutiques ciblant les enzymes de biosynthèse des glycosaminoglycanes." Thesis, Université de Lorraine, 2015. http://www.theses.fr/2015LORR0182/document.

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Les glycosyltransférases (GTs) sont une famille importante d’enzymes responsable de la biosynthèse des chaînes de glycosaminoglycane (GAG) des protéoglycanes, composants clés de la matrice extracellulaire et de la membrane plasmique cellulaire impliqués dans la communication, l'adhésion, la migration et la prolifération cellulaires. Les GTs jouent donc un rôle central dans de nombreux processus physiologiques et physiopathologiques tels que les cancers ou encore les maladies dégénératives et génétiques. Parmi ces GTs, la ß1,4-galactosyltransférase 7 (ß4GalT7) est une cible thérapeutique potent
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13

Du, Toit Therina. "An investigation into the influence of rooibos (Aspalathus linearis) on androgen metabolism in normal and prostate cancer cells." Thesis, Stellenbosch : Stellenbosch University, 2015. http://hdl.handle.net/10019.1/96926.

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Thesis (MSc)--Stellenbosch University, 2015.<br>ENGLISH ABSTRACT: In this study, the influence of rooibos on the catalytic activity of enzymes 17β -hydroxysteroid dehydrogenase type 3 (17βHSD3), 17β-hydroxysteroid dehydrogenase type 5 (AKR1C3), 17β-hydroxysteroid dehydrogenase type 2 (17βHSD2), 5α-reductase type 1 (SRD5A1) and 5α-reductase type 2 (SRD5A2), which catalyse prostate androgen metabolism, was investigated. The activities of both 17βHSD3 and AKR1C3 heterologously expressed in CHO-K1 and HEK293 cells were inhibited significantly by rooibos, with rooibos reducing the conversion of
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Schloms, Lindie. "The inhibition of adrenal steroidogenic enzymes and modulation of glucocorticoid levels in vitro and in vivo by aspalathus linearis (rooibos)." Thesis, Stellenbosch : Stellenbosch University, 2015. http://hdl.handle.net/10019.1/97000.

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Thesis (PhD)--Stellenbosch University, 2015.<br>ENGLISH ABSTRACT: This study describes: • the influence of a methanolic extract of unfermented Rooibos and five major Rooibos flavonoids, aspalathin, nothofagin, rutin, orientin and vitexin, on the activities of key adrenal steroidogenic enzymes - cytochrome P450 17β- hydroxylase/17,20-lyase (CYP17A1), 3β-hydroxysteroid dehydrogenase • the development of a novel UPLC-MS/MS method for the separation and quantification of 21 adrenal steroid metabolites; • the influence of Rooibos and aforementioned flavonoids on adrenal steroid hormone prod
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15

Camberlein, Virgyl. "Target-guided synthesis of metalloenzymes ligands with therapeutic applications." Thesis, Université de Lille (2022-....), 2022. http://www.theses.fr/2022ULILS004.

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La synthèse guidée par la cible de ligands protéiques est une stratégie innovante pour découvrir des composés bioactifs. En particulier, la Kinetic Target-Guided Synthesis (KTGS) and the Dynamic Combinatorial Chemistry (DCC) ont permis, ces dernières années, de découvrir des ligands originaux pour des cibles thérapeutiques mal explorées, ce qui a permis de lancer des projets de découverte de médicaments. Ce projet de thèse vise à utiliser la KTGS pour découvrir, puis optimiser des ligands de deux classes de métalloenzymes que sont les aminopeptidases du réticulum endoplasmiques (ERAP) et l’éla
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Roura, Frigolé Helena. "Biomedical studies of human adenosine deaminase acting on transfer RNA and related therapeutic strategies." Doctoral thesis, Universitat de Barcelona, 2018. http://hdl.handle.net/10803/650900.

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Adenosine deaminase acting on transfer RNA (ADAT) is a human heterodimeric enzyme that catalyzes the deamination of adenosine (A) to inosine (I) at the first position of the anticodon of transfer RNAs (tRNAs) (position 34, or wobble position); one of the few essential post-transcriptional modifications on tRNAs (1-5). Inosine 34 allows the recognition of three different nucleotides: cytidine, uridine and adenosine, at the third position of the codon, thus increasing the decoding capacity of tRNAs to more than one messenger RNA (mRNA) codon (adenosine 34 can in principle only pair with codons w
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Morris, Benjamin L. "Understanding and targeting the C-terminal Binding Protein (CtBP) substrate-binding domain for cancer therapeutic development." VCU Scholars Compass, 2016. http://scholarscompass.vcu.edu/etd/4434.

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Cancer involves the dysregulated proliferation and growth of cells throughout the body. C-terminal binding proteins (CtBP) 1 and 2 are transcriptional co-regulators upregulated in several cancers, including breast, colorectal, and ovarian tumors. CtBPs drive oncogenic properties, including migration, invasion, proliferation, and survival, in part through repression of tumor suppressor genes. CtBPs encode an intrinsic dehydrogenase activity, utilizing intracellular NADH concentrations and the substrate 4-methylthio-2-oxobutyric acid (MTOB), to regulate the recruitment of transcriptional regulat
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18

Chan, Ka-ho John, and 陳家豪. "Effects of Chinese green tea on cigarette smoke-induced oxidative stress, inflammation and proteases/anti-proteases in rat lung in vivo." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2010. http://hub.hku.hk/bib/B45199334.

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The Best PhD Thesis in the Faculties of Architecture, Arts, Business &Economics, Education, Law and Social Sciences (University of HongKong), Li Ka Shing Prize, 2008-2009<br>published_or_final_version<br>Medicine<br>Doctoral<br>Doctor of Philosophy
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19

Peng, Cong. "Novel Therapeutic Targets for Ph+ Chromosome Leukemia and Its Leukemia Stem Cells: A Dissertation." eScholarship@UMMS, 2010. https://escholarship.umassmed.edu/gsbs_diss/473.

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The human Philadelphia chromosome (Ph) arises from a translocation between chromosomes 9 and 22 [t(9;22)(q34;q11)]. The resulting chimeric BCR-ABLoncogene encodes a constitutively activated, oncogenic tyrosine kinase that induces chronic myeloid leukemia (CML) and B-cell acute lymphoblastic leukemia (B-ALL). The BCR-ABL tyrosine kinase inhibitor (TKI), imatinib mesylate, induces a complete hematologic and cytogenetic response in the majority of CML patients, but is unable to completely eradicate BCR-ABL–expressing leukemic cells, suggesting that leukemia stem cells are not eliminated. Over tim
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20

Pinto, Claudineia Aparecida Sales de Oliveira. "Estudo comparativo da estabilidade de formulações cosméticas contendo papaína livre e modificada." Universidade de São Paulo, 2005. http://www.teses.usp.br/teses/disponiveis/9/9139/tde-28052015-144659/.

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A papaína é uma enzima utilizada em formulações tópicas como agente proteolítico debridante, no tratamento de lesões abertas de grande extensão e queimaduras. Também empregada como agente promotor da permeação cutânea, peeling químico e como agente depilatório progressivo. A estabilidade de formulações contendo enzimas não é facilmente alcançada. No presente trabalho realizou-se a modificação da papaína com polietilenoglicol, visando maior estabilidade. O Teste de Estabilidade Normal de formulações cosméticas incorporadas de papaína não modificada e modificada apresentou um perfil diferenciado
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Gon?alves, Aline Bacelar. "Assimila??o de nitrog?nio e crescimento apical em fungos filamentosos produtores de L-asparaginase." UFVJM, 2016. http://acervo.ufvjm.edu.br/jspui/handle/1/1452.

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Submitted by Jos? Henrique Henrique (jose.neves@ufvjm.edu.br) on 2017-09-12T18:28:33Z No. of bitstreams: 2 license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5) aline_bacelar_goncalves.pdf: 5988024 bytes, checksum: 24d09b3ca0a2e58cc7aee0ca7ca2528f (MD5)<br>Approved for entry into archive by Rodrigo Martins Cruz (rodrigo.cruz@ufvjm.edu.br) on 2017-09-18T12:57:54Z (GMT) No. of bitstreams: 2 license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5) aline_bacelar_goncalves.pdf: 5988024 bytes, checksum: 24d09b3ca0a2e58cc7aee0ca7ca2528f (MD5)<br>Made available in D
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VALLONE, ALESSANDRA. "INVESTIGATION OF NOVEL THERAPEUTIC TOOLS AGAINST INFECTIOUS DISEASES Part 1. Medicinal Chemistry Investigation of MMV019918 Derivatives as Dual Schizonticide And Gametocytocidal Agents Against Plasmodium falciparum Part 2. Investigation of 5-Aryl-Heterocycles As Potential Inhibitors of Metallo beta-Lactamase Enzymes." Doctoral thesis, Università di Siena, 2017. http://hdl.handle.net/11365/1004943.

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Among infectious diseases, two large groups have great clinical relevance: parasitic and bacterial infections. Belonging to the first category is malaria, caused by the parasite Plasmodium falciparum. Transmission of Plasmodium parasites between humans and Anopheles mosquitoes is one of the most important contributors to the global impact of malaria and to the difficulties encountered in eliminating this parasite1 . Gametocytogenesis, the process by which merozoites switch from asexual replication to produce male and female gametocytes, represents a critical step in malaria transmission
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23

Canning, Peter. "The prolyl oligopeptidase family enzymes : structural basis of inhibition." Thesis, University of Warwick, 2009. http://wrap.warwick.ac.uk/2746/.

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The prolyl oligopeptidase family enzymes are a group of medically significant proteins distributed in all kingdoms of life that have several unifying structural and functional features. Members of the family hydrolyse short peptides, normally no more than 30 amino acids long. This strict substrate specificity is regulated by β-propeller domains that restrict access to the active site. Conformational changes allow access to the active site by small peptides but block access to larger, structured peptides. Mechanistic details such as these were revealed when the structure of prolyl oligopeptidas
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Alabbas, Alhumaidi B. "GLYCOSAMINOGLYCAN LYASES IN THE PREPARATION OF OLIGOSACCHARIDES." VCU Scholars Compass, 2018. https://scholarscompass.vcu.edu/etd/5279.

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Glycosaminoglycans are heterogeneous polysaccharides that mediate important biological functions. There has been considerable interest in deciphering the precise GAG sequences that are responsible for protein interactions. In fact, several GAG oligosaccharides have been discovered to date as targeting proteins with higher level of specificity. Yet, it has been difficult to develop GAG oligosaccharides as drugs. One of the key reasons for this state of art is that GAG synthesis is extremely challenging and is highly structure-specific. Thus, much of the biology and pharmacology of GAG remains u
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25

Tillotson, Joseph, and Joseph Tillotson. "Targeting Enzymes Involved in Protein Translation and Quality Control as Potential Cancer Therapeutics." Diss., The University of Arizona, 2016. http://hdl.handle.net/10150/621777.

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Activation of pathways resulting in an overexpression of oncoproteins, reliant on cap-dependent translation, or mutations of key proteins in a pathway can be advantageous to cancer cells but creates heightened protein quality control pressure. Because of this, there has been an interest in targeting enzymes involved in protein synthesis and protein quality control: such as the eukaryotic initiation factor, eIF4A, a DEAD-box RNA helicase involved in translation initiation, and p97, an AAA+ chaperone involved in protein quality control. Despite some successes in discovering both eIF4A and p97 in
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Dierenfeld, Ashley Dawn. "Enzyme replacement therapy treatment from birth increases therapeutic efficacy and generates tolerance to enzyme in canine mucopolysaccharidosis type I." [Ames, Iowa : Iowa State University], 2009. http://gateway.proquest.com/openurl?url_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:dissertation&res_dat=xri:pqdiss&rft_dat=xri:pqdiss:1473198.

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Benelkebir, Hanae. "Synthesis of cyclic peptide natural products and inhibitors of histone modifying enzymes." Thesis, University of Southampton, 2011. https://eprints.soton.ac.uk/338968/.

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Natural products have been the source of numerous leads for several drugs. As these natural products are often isolated in small quantities, it is necessary to produce them synthetically to allow testing for biological activity. Furthermore, synthesis allows the preparation of unnatural analogues for SAR studies. Cyclic peptides represent an important family of biologically active natural products. The hepta- and octacyclopeptides sanguinamide A and sanguinamide B were recently isolated in submicromolar amounts by the Molinski group. The lack of material prevented biological evaluation of the
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ageely, Eman. "Chemical Tools for Potential Therapeutic Applications of CRISPR Systems." OpenSIUC, 2020. https://opensiuc.lib.siu.edu/dissertations/1831.

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Clustered regularly interspaced short palindromic repeats (CRISPR) are derived from a bacterial and archaeal adaptive immune system. The core enzymes of CRISPR are RNA-guided endonucleases that sequence-specifically cleave foreign double-stranded DNA. Improving and controling the properties of the CRISPR system is a crucial step in advancing the therapeutic potential of CRISPR technology. Several classes of these enzymes exist and are being adapted for biotechnology, such as genome engineering. Cas12a (Cpf1) is a Type V CRISPR-associated (Cas) enzyme that naturally uses only one guide RNA, in
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Migani, D. "Proteomics Based process and cell line development applied to a mammalian therapeutic enzyme." Thesis, University College London (University of London), 2017. http://discovery.ucl.ac.uk/1565171/.

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Recombinant human Acid Alpha Glucosidase (GAA) is the therapeutic enzyme used for the treatment of Pompe disease, a rare genetic disorder characterised by GAA deficiency in the cell lysosomes. The manufacturing process for GAA can be challenging, in part due to protease degradation. The overall goal of this project was to understand the effects of GAA overexpression on cell lysosomal phenotype and host cell protein (HCP) release, and any resultant consequences for protease levels and ease of manufacture. To do this we first generated a human recombinant GAA producing stable CHO clonal cell lin
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Alyousef, Abdullah. "Identification and characterisation of lysin enzymes as potential therapeutics for the treatment of Clostridium difficile." Thesis, Cardiff University, 2013. http://orca.cf.ac.uk/49926/.

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Clostridium difficile is the most common cause of hospital acquired infections. While the current treatments of choice, antibiotics, are generally effective in promoting recovery ,the increased incidence of C. difficile infections and treatment failure associated with antibiotic resistance combined with the emergence of hypervirulent strains highlights the need to develop therapeutic approaches that specifically target the pathogen without causing collateral damage to the protective microbiota. Several non-antibiotic approaches are currently being investigated, such as bacteriophage therapy. F
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Page, Simon Matthew. "Ruthenium anticancer complexes : a targeted approach to enzyme inhibition." Thesis, University of Cambridge, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.608027.

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Broek, Stanislaus Antonius Jacobus van den. "Angiotensin-converting enzyme inhibitors in heart failure clinical end points to assess therapeutic efficacy /." [S.l. : [Groningen : s.n.] ; University Library Groningen] [Host], 1994. http://irs.ub.rug.nl/ppn/293017212.

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Cheng, Feng Verfasser], Ulrich [Akademischer Betreuer] [Schwaneberg, and Lothar [Akademischer Betreuer] Elling. "Protein engineering of a therapeutic enzyme arginine deiminase / Feng Cheng ; Ulrich Schwaneberg, Lothar Elling." Aachen : Universitätsbibliothek der RWTH Aachen, 2015. http://d-nb.info/1127232053/34.

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Cheng, Feng [Verfasser], Ulrich [Akademischer Betreuer] Schwaneberg, and Lothar [Akademischer Betreuer] Elling. "Protein engineering of a therapeutic enzyme arginine deiminase / Feng Cheng ; Ulrich Schwaneberg, Lothar Elling." Aachen : Universitätsbibliothek der RWTH Aachen, 2015. http://d-nb.info/1127232053/34.

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Ehren, Jennifer. "Identifying and engineering the best oral enzyme therapy for celiac sprue : two therapeutic options /." May be available electronically:, 2008. http://proquest.umi.com/login?COPT=REJTPTU1MTUmSU5UPTAmVkVSPTI=&clientId=12498.

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Pennington, Oliver John. "The development of molecular tools for the expression of prodrug converting enzymes in Clostridium sporogenes." Thesis, University of Nottingham, 2006. http://eprints.nottingham.ac.uk/13295/.

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Despite intensive research, cancer remains one of the major causes of worldwide morbidity. It is widely believed, however, that if currently available anti-cancer drugs could be delivered specifically to tumours then the disease would have been mastered. The delivery of prodrug converting enzymes by clostridial spores specifically to the anoxic centres of tumours is one potential delivery mechanism. This is due to the extreme selectivity of spores to germinate solely in the hypoxic regions of tumours. Once germinated, the expression of a prodrug converting enzyme converts a systemical1y admini
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Girnita, Leonard. "Growth factor pathways in human cancer : functional and therapeutic implications /." Stockholm, 2002. http://diss.kib.ki.se/2002/91-7349-307-4.

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Prabhakar, Vikas. "Therapeutics discovery via glycotechnology : the development of protein engineered enzymes for the study of galactosaminoglycan neuromedicine." Thesis, Massachusetts Institute of Technology, 2006. http://hdl.handle.net/1721.1/38917.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Biological Engineering Division, 2006.<br>"June 2006."<br>Includes bibliographical references.<br>Glycans are chemically heterogeneous macromolecules that have profound importance in a variety of biological processes. Located at the surfaces of cells, deposited in the extracellular matrix, or attached to soluble signaling agents, these molecules are characterized by a structural complexity that has thus far prevented their widespread exploitation in biomedicine. Insight into the fine structure and sequence of these complex biomolecules pr
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Leman, Géraldine. "Régulation de la fonction mitochondriale par le rapport NADH/NAD+ : le rôle clef du complexe I." Thesis, Angers, 2014. http://www.theses.fr/2014ANGE0016/document.

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Le NAD+ apparaît comme un régulateur majeur du fonctionnement mitochondrial. En effet, ce cofacteur régule non seulement l’activité de nombreuses enzymes impliqués dans le métabolisme énergétique (enzymes de la β-oxydation des acides gras, du cycle de Krebs) mais joue également un rôle dans la production d’espèces réactives de l’oxygène (ROS). Le NAD+ est aussi le cofacteur des sirtuines, des enzymes déacétylases régulatrices notamment du métabolisme mitochondrial. De plus, la mitochondrie est l’organite au sein duquel la concentration en NAD+ est la plus élevée (jusqu’à 70% du NAD cellulaire)
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Chen, Xiabin. "DEVELOPMENT OF COCAINE HYDROLASE FOR THERAPEUTIC TREATMENT OF COCAINE ABUSE." UKnowledge, 2016. http://uknowledge.uky.edu/pharmacy_etds/59.

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Cocaine abuse is a world-wide public health and social problem without a U.S. Food and Drug Administration (FDA)-approved medication. An ideal anti-cocaine medication would accelerate cocaine metabolism producing biologically inactive metabolites by administration of an efficient cocaine-specific exogenous enzyme. Recent studies in our lab have led to discovery of the desirable, highly efficient human cocaine hydrolases (hCocHs) that can efficiently detoxify and inactivate cocaine without affecting normal functions of central nervous system (CNS). Preclinical and clinical data have demonstrate
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Schuler, Aaron D. "Development of sirtuin and calmodulin-dependent protein kinase inhibitors as anti-cancer therapeutics /." Thesis, Connect to this title online; UW restricted, 2006. http://hdl.handle.net/1773/8491.

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Wagner, Jonathan Mark. "STRUCTURAL BASIS OF SUBSTRATE RECOGNITION IN THIMET OLIGOPEPTIDASE AND DEVELOPMENT OF NANOPARTICLES FOR THERAPEUTIC ENZYME DELIVERY." UKnowledge, 2012. http://uknowledge.uky.edu/biochem_etds/6.

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Neuropeptidases are responsible for degradation of signaling peptides in the central nervous system and periphery. Some neuropeptidases have also been shown to play a role as part of the cell’s hydrolytic machinery responsible for breaking down proteins and peptides into amino acids, and these enzymes therefore influence small peptide availability for antigen presentation. A better understanding of how neuropeptidases recognize their substrates could lead to therapeutics that modulate the activity of these important enzymes. Alternatively, re-engineering these enzymes to selectively hydrolyze
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43

Maianti, Juan Pablo. "Therapeutic potential and physiological roles of Insulin-Degrading Enzyme illuminated by a DNA-templated macrocyclic inhibitor." Thesis, Harvard University, 2015. http://nrs.harvard.edu/urn-3:HUL.InstRepos:17467523.

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Insulin-Degrading Enzyme (IDE) is a zinc-metalloprotease responsible for the clearance of insulin in peripheral tissues. Despite decades of speculation that inhibiting endogenous insulin degradation might treat Type-2 Diabetes, the functional relationship between IDE and glucose homeostasis remains unclear. IDE inhibitors that are active in vivo are therefore needed to elucidate IDE’s physiological roles and to determine its potential to serve as a target for the treatment of diabetes. In this thesis I describe the development of the first highly specific IDE in vivo probe, identified from
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44

Yang, Seung Ook. "Enzyme Encapsulation, Biosensing Endocrine Disrupting Chemicals, and Bio-therapeutic Expression Platforms Using Cell-Free Protein Synthesis." BYU ScholarsArchive, 2017. https://scholarsarchive.byu.edu/etd/6885.

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Cell-free protein synthesis (CFPS) is a powerful protein expression platform where protein synthesis machinery is borrowed from living organisms. Target proteins are synthesized in a reaction tube together with cell extract, amino acids, energy source, and DNA. This reaction is versatile, and dynamic optimizations of the reaction conditions can be performed. The "œopen" nature of CFPS makes it a compelling candidate for many technologies and applications. This dissertation reports new and innovative applications of CFPS including 1) enzyme encapsulation in a virus-like particle, 2) detection
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45

Ho, Kwun-wai, and 何冠威. "Angiotensin converting enzyme inhibitor alone or in combination with angiotensin II type I receptor blocker in patients with chronicproteinuric nephropathies: a systemic reviewof clinical trials." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2005. http://hub.hku.hk/bib/B45010687.

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46

Seed, Alison. "Characterisation of the pharmacological actions in humans of multiple vasoactive enzyme inhibitors with therapeutic potential in heart failure." Thesis, Connect to e-thesis, 2007. http://theses.gla.ac.uk/119/.

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Thesis (M.D.) - University of Glasgow, 2007.<br>M.D. thesis submitted to the Faculty of Medicine, Dept. of Medicine and Therapeutics, University of Glasgow, 2007. Includes bibliographical references. Print version also available.
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Brice, Edmund Andrew William. "Rat angiotensin-converting enzyme : tissue specific expression during pharmacological inhibition." Doctoral thesis, University of Cape Town, 1995. http://hdl.handle.net/11427/27042.

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The renin-angiotensin system plays a central role in the maintenance of blood pressure. Angiotensin II, the main effector of this system, results from the action of angiotensin-converting enzyme (ACE) on angiotensin I. Angiotensin II, maintains vasomotor tone via its vasoconstrictor action, and also increases salt and water retention by stimulating the release of aldosterone. ACE inhibitors, such as captopril, enalapril and lisinopril, are highly effective in the treatment of hypertension and congestive cardiac failure. Previous studies have suggested that angiotensin converting enzyme (ACE) p
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Regan, Nicholas Bauman. "The Design and Synthesis of Small Molecule Protein Inhibitors as Potential Cancer Therapeutics." The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1303823563.

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Harun, Norlida. "Application of molecularly imprinted solid phase extraction, enzyme-linked immunosorbent assay and liquid chromatography tandem mass spectrometry to forensic toxicology." Thesis, University of Glasgow, 2010. http://theses.gla.ac.uk/1992/.

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The rapid growth of ketamine and amphetamine misuse worldwide has led to the development of methods for the detection and analysis of ketamine and amphetamines in biological specimens. Most methods previously developed in forensic toxicology for the detection of ketamine and amphetamines used GC-MS. The present work developed alternative methods based on LC-MS/MS. Ketamine was chosen as the drug of interest because there are no data currently available on the extent of ketamine abuse in Malaysia even though a large amount of ketamine has been seized by the Malaysian Royal Police, while ampheta
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Chettiar, Somsundaram Natrajan. "Design and Synthesis of Small Molecules as Potential Therapeutic Agents for the Treatment of Cancer and Cystic Fibrosis." The Ohio State University, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=osu1385559040.

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